Back to results
US 2026/0306650 A1Published application
Camptothecin drug conjugate and use thereof
AssigneeShanghai Zaimo Biotechnology Co., Ltd.
InventorDapeng SUN
Life of this patent
Estimating the term…
Abstract
Disclosed are a camptothecin drug conjugate and a use thereof. The present disclosure provides a drug conjugate of formula II or a pharmaceutically acceptable salt thereof. The camptothecin drug conjugate provided by the present disclosure has a good inhibitory effect on ovarian cancer, breast ductal carcinoma, breast cancer, pancreatic adenocarcinoma, pancreatic cancer or gastric cancer.
Claims14
A drug conjugate of formula II or a pharmaceutically acceptable salt thereof,
- wherein
- Ab is an antibody or an antigen-binding fragment thereof,
- GT is a group connected to an antibody or an antigen-binding fragment thereof,
- GL is a single bond or a linking group;
- wherein GE is connected to GL;
- each GE is independently a polypeptide residue consisting of
- and t amino acid residues, each of the amino acid residues is independently a natural amino acid residue or a non-natural amino acid residue, and t is an integer of 1-10;
- Z1 and Z2 are independently —CH2— or O;
- GF and GS are a self-immolative group;
- G1 is
- each Rc is independently C1-6 alkyl;
- each Rc1 is independently
- each Rd is independently carboxyl,
- each Rd1 is independently H or C1-6 alkyl;
- m5 and m6 are each independently 1, 2, 3, 4, 5 or 6;
- Am is a single bond, a natural amino acid residue or a non-natural amino acid residue;
- D is
- X1 is NH or O;
- A is H, halogen, hydroxyl, amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C6-10 aryl, 5- to 10-membered heteroaryl, C3-6 cycloalkyl or 3- to 6-membered heterocyclyl;
- RA, RB and RC are independently H, halogen, hydroxyl, amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C6-10 aryl, 5- to 10-membered heteroaryl, C3-6 cycloalkyl or 3- to 6-membered heterocyclyl;
- or, any two of RA, RB and RC together with the silicon atom to which they are attached form a C5-6 cycloalkyl ring or a 5- to 6-membered heterocyclyl ring, and the 5- to 6-membered heterocyclyl optionally further comprises one, two or three types of heteroatoms selected from N, O and S, and the number of the heteroatoms in the 5- to 6-membered heterocyclyl is independently 1, 2 or 3;
- X is O or S;
- n1 and n2 are independently 0, 1, 2 or 3;
- z is an integer or decimal of 1-16;
- 5- to 10-membered heteroaryl and 3- to 6-membered heterocyclyl each comprise one, two or three types of heteroatoms selected from N, O and S, and the number of the heteroatoms is independently 1, 2 or 3.
22 more elements
Dependencies are inferred from the claim text.